RG7388 is the second generation inhibitor of P53-MDM2 interaction. It is orally active, potently and selectively antagonizing the P53-MDM2 interaction with Ki at low nM. Highly optimized from pyrrolidin-based derivatives, RG7388 represents a distinctive, brand-new structural category of MDM2 ligand, a significant departure from the nutlin-based, first generation ligands exemplified by RG7112. Like RG7112, RG7388 binds selectively to the p53 site on the surface of the MDM2 molecule, effectively displacing p53 from MDM2, leading to p53 stabilization and activation of the p53 pathway. However, RG7388, as compared with its predecessor, binds to the MDM2 protein with a higher potency and selectivity, and has substantially improved pharmacological properties and superior clinical efficacy at lower doses and exposures.

KEYWORDS: RG-7388 | Supplier | MDM2 antagonist | Idasanutlin | RO5503781 | RG7388 | RG 7388 | RO-5503781 | RO 5503781 | CT-RG7388 | CAS [1229705-06-9] | p53 | HDM-MDM | Antagonist | Enzymes